Application of chitosan nanoparticle served as drug delivery system for cancer therapy / 中国临床药理学与治疗学

Cancer is one of the malignant diseases threatening human. In recent years, nanotechnology is becoming the hope the cancer treatment, as it can take the drugs targeting to tumor sites, with enhanced efficacy and reduced toxicity. Chitosan is the only alkaline polysaccharide in nature with good biocompatibility and biodegradability. Moreover, chitosan has many reaction sites to make derivatives with different properties. Chitosan and its derivatives are widely used for drug delivery systems and tissue engineering scaffolds. Hence, they are valuable in the field of biomedicine. In this paper, the recent advances chitosan nanoparticles as drug delivery system for delivering anticancer drugs are reviewed, especially the advances of the preparation, passive targeting, active targeting, and stimuli-responsive drug delivery systems of chitosan nanoparticles.

monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET

Microemulsions are promising drug delivery systems for the oral administration of poorly water-soluble drugs. However, the evolution of microemulsions in the gastrointestinal tract is still poorly characterized, especially the structural change of microemulsions under the effect of lipase and mucus. To better understand the fate of microemulsions in the gastrointestinal tract, we applied small-angle X-ray scattering (SAXS) and fluorescence resonance energy transfer (FRET) to monitor the structural change of microemulsions under the effect of lipolysis and mucus. First, the effect of lipolysis on microemulsions was studied by SAXS, which found the generation of liquid crystalline phases. Meanwhile, FRET spectra indicated micelles with smaller particle sizes were generated during lipolysis, which could be affected by CaCl, bile salts and lecithin. Then, the effect of mucus on the structural change of lipolysed microemulsions was studied. The results of SAXS and FRET indicated that the liquid crystalline phases disappeared, and more micelles were generated. In summary, we studied the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET, and successfully monitored the appearance and disappearance of the liquid crystalline phases and micelles.

Research Progress in Multiple Target Action Mechanisms of Myocardium of Exogenous Phosphocreatine / 医药导报

Phosphocreatine ( PCr), a natural high energy phosphate, plays a pivotal role in maintaining energy homeostasis of the body. Exogenous PCr has been developed as a cardio-protective drug and extensively used in treatment of cardiovascular diseases.PCr has special chemical structure,which confers much bioinformation on it,and becomes a multitarget-directed drug.Since the 21st century,with rapid development of molecular biology,the multiple target action mechanisms of PCr have continually gained elucidation,including energy-related and non-energy-related mechanisms,intracellular and extracellular mechanisms,which are leading to its extensive clinical applications in cardiovascular diseases.Based on author' s research and published literatures,this article reviews the research progress in multiple target action mechanisms of PCr,including energy supply,membrane stabilization, anti-platelet aggregation, electrophysiology, enzyme inhibition and protection of mitochondria, antiapoptotic effect,etc.

Ameliorative effects of atractylodin on intestinal inflammation and co-occurring dysmotility in both constipation and diarrhea prominent rats

Intestinal disorders often co-occur with inflammation and dysmotility. However, drugs which simultaneously improve intestinal inflammation and co-occurring dysmotility are rarely reported. Atractylodin, a widely used herbal medicine, is used to treat digestive disorders. The present study was designed to characterize the effects of atractylodin on amelioration of both jejunal inflammation and the co-occurring dysmotility in both constipation-prominent (CP) and diarrhea-prominent (DP) rats. The results indicated that atractylodin reduced proinflammatory cytokines TNF-α, IL-1β, and IL-6 in the plasma and inhibited the expression of inflammatory mediators iNOS and NF-kappa B in jejunal segments in both CP and DP rats. The results indicated that atractylodin exerted stimulatory effects and inhibitory effects on the contractility of jejunal segments isolated from CP and DP rats respectively, showing a contractile-state-dependent regulation. Atractylodin-induced contractile-state-dependent regulation was also observed by using rat jejunal segments in low and high contractile states respectively (5 pairs of low/high contractile states). Atractylodin up-regulated the decreased phosphorylation of 20 kDa myosin light chain, protein contents of myosin light chain kinase (MLCK), and MLCK mRNA expression in jejunal segments of CP rats and down-regulated those increased parameters in DP rats. Taken together, atractylodin alleviated rat jejunal inflammation and exerted contractile-state-dependent regulation on the contractility of jejunal segments isolated from CP and DP rats respectively, suggesting the potential clinical implication for ameliorating intestinal inflammation and co-occurring dysmotility.

Research progress on the protection of tetramethylpyrazine in different kinds of damage of nervous system and its mechanisms / 中国药理学通报

Tetramethylpyrazine(TMP)is a main active alkaloid ingredient of Traditional Chinese Medicine Ligusticum chuanqiong Hort. The article reviews the protection of TMP against pathological damage and nervous retardation disease in central nervous and peripheral nervous system and summarizes the mechanisms in basic research,clinical practice and so on.

Characteristics of inverse agonist action / 中国药理学通报

Inverse agonist is a new type of classification.Different form antagonist that blocks the effect of agonist,inverse agonist produces opposite effect to that of agonist.The characteristics of inverse agonists acting on different receptors including H_2,H_3,? opioid,adrenergic ?, and 5-HT_((1B)) receptors are discussed in this paper.Recent investigation suggested that inverse agonist has potential clinical application.